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Cancer Chemotherapy and Pharmacology

Erschienen in:

01.03.2012 | Original Article

Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice

verfasst von: Liu Zhongfa, Ming Chiu, Jiang Wang, Wei Chen, Winston Yen, Patty Fan-Havard, Lisa D. Yee, Kenneth K. Chan

Erschienen in: Cancer Chemotherapy and Pharmacology | Ausgabe 3/2012

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Abstract

Purpose

Curcumin has shown a variety of biological activity for various human diseases including cancer in preclinical setting. Its poor oral bioavailability poses significant pharmacological barriers to its clinical application. Here, we established a practical nano-emulsion curcumin (NEC) containing up to 20% curcumin (w/w) and conducted the pharmacokinetics of curcuminoids and curcumin metabolites in mice.

Methods

This high loading NEC was formulated based on the high solubility of curcumin in polyethylene glycols (PEGs) and the synergistic enhancement of curcumin absorption by PEGs and Cremophor EL. The pharmacokinetics of curcuminoids and curcumin metabolites was characterized in mice using a LC–MS/MS method, and the pharmacokinetic parameters were determined using WinNonlin computer software.

Results

A tenfold increase in the AUC _0→24h and more than 40-fold increase in the C _max in mice were observed after an oral dose of NEC compared with suspension curcumin in 1% methylcellulose. The plasma pharmacokinetics of its two natural congeners, demethoxycurcumin and bisdemethoxycurcumin, and three metabolites, tetrahydrocurcumin (THC), curcumin-O-glucuronide, and curcumin-O-sulfate, was characterized for the first time in mice after an oral dose of NEC.

Conclusion

This oral absorption enhanced NEC may provide a practical formulation to conduct the correlative study of the PK of curcuminoids and their pharmacodynamics, e.g., hypomethylation activity in vivo.

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Titel: Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice
verfasst von: Liu Zhongfa
Ming Chiu
Jiang Wang
Wei Chen
Winston Yen
Patty Fan-Havard
Lisa D. Yee
Kenneth K. Chan
Publikationsdatum: 01.03.2012
Verlag: Springer-Verlag
Erschienen in: Cancer Chemotherapy and Pharmacology / Ausgabe 3/2012
Print ISSN: 0344-5704
Elektronische ISSN: 1432-0843
DOI: https://doi.org/10.1007/s00280-011-1749-y

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Springer Medizin

Enhancement of curcumin oral absorption and pharmacokinetics of curcuminoids and curcumin metabolites in mice

Abstract

Purpose

Methods

Results

Conclusion

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Springer Medizin

Abstract

Purpose

Methods

Results

Conclusion

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